| S7158 |
LY2835219 |
LY2835219 is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM, respectively. Phase 3. |
Pan |
CDK6, IC50: 10 nM |
| S1116 |
Palbociclib (PD-0332991) HCl |
Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3. |
Pan |
CDK6/CyclinD2, IC50: 15 nM |
| S1579 |
Palbociclib (PD0332991) Isethionate |
Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3. |
Pan |
CDK6/CyclinD2, IC50: 15 nM |
| S1230 |
Flavopiridol (Alvocidib) |
Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2. |
Pan |
CDK6, IC50: 40 nM |
| S2679 |
Flavopiridol (Alvocidib) HCl |
Flavopiridol HCl competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2. |
Pan |
CDK6, IC50: 40 nM |
| S1524 |
AT7519 |
AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. Phase 2. |
Pan |
CDK6/CyclinD3, IC50: 170 nM |
| S1249 |
JNJ-7706621 |
JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1. |
Pan |
CDK6/CyclinD1, IC50: 175 nM |
| S8058 |
P276-00 |
P276-00 is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Phase 2/3. |
Pan |
CDK6/CyclinD3, IC50: 396 nM |
| S7440 |
LEE011 |
LEE011 is an orally available, and highly specific CDK4/6 inhibitor. Phase 3. |
Pan |
|